Cas No.: | 623152-17-0 |
Chemical Name: | BMS 582949 |
Synonyms: | BMS 582949;4-[5-(cyclopropylcarbamoyl)-2-methylanilino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide;38P;3mvl;UNII-CR743OME9E |
SMILES: | O=C(C1=CN2N=CN=C(NC3=CC(C(NC4CC4)=O)=CC=C3C)C2=C1C)NCCC |
Formula: | C22H26N6O2 |
M.Wt: | 406.48084 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | BMS-626529 is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells. |
In Vitro: | BMS-626529 has half-maximal effective concentration (EC50) values of <10 nM against the vast majority of viral isolates. BMS-626529 exhibits an average EC50 against LAI virus of 0.7±0.4 nM. BMS-626529 exhibits an EC50 of 0.01 nM against the most susceptible virus and an EC50 of >2,000 nM against the least susceptible virus. The cytotoxicity profile of BMS-626529 is examined in several cell types from different human tissues. CC50 values of >200 μM are observed in MT-2 (T lymphocytes), HEK293 (kidney), HEp-2 (larynx), HepG2 (liver), HeLa (cervix), HCT116 (colorectal), MCF-7 (breast), SK-N-MC (neuroepithelium), HOS (bone), H292 (lung), and MDBK (bovine kidney) cells measured after 3 or 6 days in culture. CC50 values of 105 and 192 μM are obtained in the T-cell line PM1 and in PBMCs, respectively, following 6 days in culture. These results show that BMS-626529 exhibits low cytotoxicity in cell culture[1]. BMS-626529 exhibits a broad spectrum of antiviral activity against a panel of clinical isolates, with a 50% inhibitory concentration (IC50) ranging from subnanomolar levels to >0.1 µM[2]. |